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Liquid pharmaceutical composition containing echinocandin antifungal agent caspofungin

A composition and antifungal technology, applied in stabilizers, can solve problems such as increasing production cost, affecting production efficiency, increasing the risk of drug use, etc.

Inactive Publication Date: 2012-08-01
SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the above-mentioned compositions are all freeze-dried products, the production process is relatively complicated, the energy consumption is high, the energy consumption of the freeze-drying process is high, the production cycle is long, and factors such as the limited freeze-drying area of ​​the freeze-dryer directly affect the production efficiency. increased production costs
And in the process of medication, reconstitution is required, which is not only inconvenient to operate, but also increases the risk of medication

Method used

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  • Liquid pharmaceutical composition containing echinocandin antifungal agent caspofungin
  • Liquid pharmaceutical composition containing echinocandin antifungal agent caspofungin
  • Liquid pharmaceutical composition containing echinocandin antifungal agent caspofungin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0062] Dissolve 1.20g of trehalose in 3ml of water, then add 7.5μl of glacial acetic acid, adjust the pH to 5.1 with 1M sodium hydroxide, then add 0.223g of caspofungin acetate, stir gently to dissolve, and oxidize with 1M hydroxide Adjust the pH to 6.0 with sodium, add water to constant volume to 5mL, and filter through a 0.22 μm membrane. The composition of the composition (Formulation 2) is as follows:

[0063] Caspofungin acetate (by base) 40mg / ml

[0064] Trehalose 240mg / ml

[0065] Glacial acetic acid 1.5mg / ml

[0066] Sodium hydroxide Adjust to pH6.0

[0067] The prepared solution was divided into 2mL antibiotic bottles according to 0.5mL / bottle, fully stoppered with rubber stoppers, capped, and placed under the conditions of 40°C, 75%RH and 30°C, 65%RH respectively for stability investigation , and samples were taken for HPLC analysis after 8 weeks.

Embodiment 3

[0069] The preparation process is similar to Example 2, except that in the preparation process, the stabilizing agent is selected between trehalose, sucrose or the composition of trehalose and sucrose, and the pH regulator used is between acetate, phosphate or citric acid Choose between salt, even do not add any additional pH adjuster, thus obtain different formulations, the composition of each composition formulation is as follows:

[0070]

[0071] The compositions of each formula were also subjected to the stability investigation described in Example 2.

Embodiment 4

[0073] After the samples of Comparative Example 1, Example 2 and Example 3 were tested for stability, the active substances were analyzed by HPLC.

[0074] The results of the 40°C stability test are shown in the table below:

[0075] recipe number

[0076] The results of the stability test at 30°C are shown in the table below:

[0077] recipe number

[0078] It can be seen from the data in the above table that the stability of the liquid composition formulation is significantly better than that of the freeze-dried composition of formulation 1, especially when the content of the stabilizer reaches a certain concentration. The HPLC chromatogram after the stability investigation of formula 1 and formula 5 is shown in the attachment Figure 1~4 .

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Abstract

The invention discloses a liquid pharmaceutical composition containing echinocandin antifungal agent caspofungin, wherein the pharmaceutical composition containing carbohydrate as a stabilizer. The pharmaceutical composition provided by the invention has good stability.

Description

technical field [0001] The present invention relates to liquid pharmaceutical compositions for the treatment and / or prevention of fungal infections. More specifically, the present invention relates to caspofungin or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable amount of a stabilizer, such as monosaccharide, disaccharide or polysaccharide, or a combination thereof. It is a liquid composition. Background technique [0002] Echinocandin, also known as echinocandin, is a new type of antifungal drug, belonging to the acetylhexacyclic group, and is a glucan synthase inhibitor, which non-competitively inhibits the -β(1,3) of the fungal cell wall -D-glucan synthesis to play a bactericidal effect. Dextran is a fungal cell wall polysaccharide and an important component of the cell wall, which can maintain the integrity of the cell wall and stabilize its osmotic pressure. [0003] Caspofungin (caspofungin) (Caseis, Merck & Co.) is the first listed pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/12A61K9/00A61K47/26A61P31/10
Inventor 洪云海薛颖季晓铭
Owner SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
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